𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Radiosynthesis and PET studies of [11C]RJR-2403, a nicotinic agonist

✍ Scribed by Andrei R. Studenov; Adam M. Wegner; Yu-Shin Ding

Publisher
John Wiley and Sons
Year
2001
Tongue
French
Weight
121 KB
Volume
44
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

(E)‐N‐methyl‐4‐(3‐pyridinyl)‐3‐butene‐1‐amine (RJR‐2403, or metanicotine), a nicotinic agonist developed as a cognitive‐enhancing drug for Alzheimer's disease, was labeled with carbon‐11 using [^11^C]methyl iodide via a simple and efficient one‐step procedure. Regioselectivity of [^11^C]methylation on the aliphatic nitrogen versus pyridine nitrogen is strongly dependent on the reaction solvent. The reaction in acetonitrile exclusively yields aliphatic N‐[^11^C‐methyl]alkylation ([^11^C]RJR‐2403), while only a byproduct is formed when DMF is used as a solvent. Positron emission tomographic (PET) studies in baboon showed a homogeneous distribution of radioactivity within baboon brain with a slow clearance. [^11^C]RJR‐2403 was metabolized very rapidly as evidenced by the fact that at 2 min after intravenous injection only 50% of the total carbon‐11 in plasma is parent compound. Copyright © 2001 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

A two-step one-pot radiosynthesis of the
A two-step one-pot radiosynthesis of the potent dopamine D2/D3 agonist PET radioligand [11C]MNPA
✍ C. Steiger; S. J. Finnema; L. Raus; M. Schou; R. Nakao; K. Suzuki; V. W. Pike; H 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 French ⚖ 295 KB

## Abstract (__R__)‐(−)‐2‐[^11^C]Methoxy‐__N__‐__n__‐propylnorapomorphine ([^11^C]MNPA ([^11^C]2)) is an agonist radioligand of interest for imaging D~2~/D~3~ receptors __in vivo__. Here we sought to develop an improved radiosynthesis of this radioligand. Reference 2 was synthesized in nine steps w

Synthesis and 11C-labelling of two selec
Synthesis and 11C-labelling of two selective high affinity nicotinic cholinergic agonists for evaluation as radioligands for PET studies
✍ Frédéric Dolle; Lilian Dolci; Héric Valette; Michel Bottlaender; Denis Fournier; 📂 Article 📅 1996 🏛 John Wiley and Sons 🌐 French ⚖ 692 KB

ABT-418 ((S)-3-methyl-5-[l-methyl-2-pyrrolidinyl]isoxazole) and N-methylcytisine (N-methyl-1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido-[ I,2-a][ 1,5]diazocin-8-one) are two high affinity nicotinic cholinergic agonists. ABT-418 was synthesized in 7 steps from commercially available (S)-Boc-proline in

Synthesis of [11C]-S21007 a novel 5HT3 p
Synthesis of [11C]-S21007 a novel 5HT3 partial agonist as a potential tracer for PET studies
✍ S. Guillouet; L. Barre; F. Gourand; M. C. Lasne; S. Rault 📂 Article 📅 1996 🏛 John Wiley and Sons 🌐 French ⚖ 187 KB 👁 1 views

A novel selective and partial agonist S21007 (IC% =InM), for 5HT3 receptor studies in positron emission tomography, has been labelled with ("Cjbenzyl iodide in 40-50% radiochemical yield and 200-700mCilpmol in 60 min synthesis time.